HA-1077
- 貨號 Cat. No.
- H-220
- 規格 Size
- 5 mg 5x5 mg 10 mg
Description
HA-1077
Rho/Rok Inhibitor
| Product#: | H-220 |
| Sizes: |
| 5 mg |
| 5 x 5 mg |
| 10 mg |
| M.W.: | 364.30 |
| CAS No.: | [103745-39-7] |
| Structure: |
 |
| Purity: | >99% |
| Bioassay: |
| HA-1077 inhibits the phosphorylation of Myosin Light Chain (MLC). |
 |
| C2C12 cells were grown in Fetal Calf Serum (FCS) until 2 days post confluence. Differentiation to myocytes was induced by 2% Horse Serum (HS) in the presence or absence of 20 mM HA-1077 for the indicated times. The cell proteins were analyzed by Western blotting using anti phospho-MLC antibody. |
| References: |
1. | Asano, T. et al. (1989) Br. J. Pharmacol. 98, 1091. |
2. | Uehata, M. et al. (1997) Nature 389, 990. |
3. | Nagumo, H. et al.(2000) Am. J. Physiol. Cell Physiol. 278, C57. |
4. | Shirotani, M. et al. (1991) J. Pharmacol. Exp. Ther. 259, 738. |
5. | Sasaki, Y. et al. (1987) Am. J. Physiol. 253, C71. |
6. | Seto, M. et al. (1991) Eur. J. Pharmacol. 195, 267. |
7. | Asano, T. et al. (1987) J. Pharmacol. Exp. Ther. 241, 1033. |
8. | Takayasu, M. et al. (1986) J. Neurosurg. 65, 80. |
9. | Takizawa, S. et al. (1993) Eur. J. Pharmacol. 250, 431. |
HA-1077 is a small, cell permeable derivative of isoquinoline which specifically inhibits the small GTPase - Rho by inhibition of its associated kinase-Rho dependent kinase (ROK). This signaling pathway acts as a molecular switch to control cytoskeleton organization in many cell types including smooth muscle.1-3 By inhibition of ROK, HA-1077 decreases the myosin light chain (MLC) phosphorylation induced by Ca2+ due to abrogating Rho-mediated inhibition of MLC dephosphorylation. HA-1077 also inhibits fetal calf serum-induced proliferation and [3H]thymidine incorporation into DNA of growth-arrested VSMC in a dose-dependent manner.4-6 At concentrations higher than 5 mM, it induces disorganization of actin filament structure. This compound was also found to act as a vasodilator and antivasospasm drug which antagonizes the verapamil-insensitive voltage dependent Ca2+ channel and is used clinically for treatment of the cerebral vasospasm after subarachnoid hemorrhage.7-9